公开(公告)号：US07923462B2

公开(公告)日：2011-04-12

申请号：US12810275

申请日：2008-12-22

申请人： Takehiro Ishikawa ,  Hitoshi Inoue ,  Satoko Kobayashi ,  Masako Yoshida ,  Hiroaki Shiohara ,  Yasunori Ueno ,  Nobuyuki Tanaka

发明人： Takehiro Ishikawa ,  Hitoshi Inoue ,  Satoko Kobayashi ,  Masako Yoshida ,  Hiroaki Shiohara ,  Yasunori Ueno ,  Nobuyuki Tanaka

IPC分类号： A61K31/4245 ,  A61K31/427 ,  C07D271/06 ,  C07D413/04 ,  C07D417/10 ,  A61P25/16

CPC分类号： C07D271/06 ,  C07D413/04 ,  C07D413/10 ,  C07D417/10

摘要： The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is halo-lower alkyl, lower acyl, halo-lower alkylcarbonyl, cycloalkylcarbonyl, optionally substituted arylcarbonyl, lower alkoxycarbonyl or the like; R4 is lower alkyl, halo-lower alkyl, cycloalkyl, lower alkoxy-lower alkyl or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

摘要翻译： 本发明提供由通式（I）表示的化合物或其药学上可接受的盐，其中R 1和R 2各自为氢，低级酰基，低级烷氧基羰基等; 低级酰基，卤代低级烷基羰基，环烷基羰基，任意取代的芳基羰基，低级烷氧基羰基等; R4是表现出强大的COMT抑制活性的低级烷基，卤代低级烷基，环烷基，低级烷氧基 - 低级烷基等。 本发明还提供含有所述化合物的药物组合物及其用途。

公开(公告)号：US20110172208A1

公开(公告)日：2011-07-14

申请号：US13002475

申请日：2009-06-26

申请人： Takehiro Ishikawa ,  Satoko Kobayashi ,  Hitoshi Inoue ,  Yasunori Ueno ,  Masako Yoshida ,  Nobuyuki Tanaka

发明人： Takehiro Ishikawa ,  Satoko Kobayashi ,  Hitoshi Inoue ,  Yasunori Ueno ,  Masako Yoshida ,  Nobuyuki Tanaka

IPC分类号： A61K31/55 ,  C07D211/08 ,  C07C233/00 ,  C07D207/00 ,  C07D265/30 ,  C07D223/04 ,  C07D241/04 ,  A61K31/445 ,  A61K31/165 ,  A61K31/40 ,  A61K31/5375 ,  A61K31/4965 ,  A61K31/195 ,  A61P25/16

CPC分类号： C07C205/61 ,  A61K31/192 ,  A61K31/24 ,  A61K31/277 ,  A61K31/351 ,  A61K31/381 ,  A61K31/40 ,  A61K31/42 ,  A61K31/425 ,  A61K31/4453 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/55 ,  A61K45/06 ,  C07C255/56 ,  C07C255/57 ,  C07C259/10 ,  C07C2601/14 ,  C07C2601/18 ,  C07D261/08 ,  C07D277/24 ,  C07D295/10 ,  C07D309/06 ,  C07D333/22 ,  A61K2300/00

摘要： The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

摘要翻译： 本发明提供由通式（I）表示的化合物或其药学上可接受的盐，其中R 1和R 2各自为氢，低级酰基，低级烷氧基羰基等; R 3是低级烷基，卤素 - 低级烷基，环烷基，杂环烷基，任选取代的芳基，任选取代的杂芳基等; R4是氰基，低级烷氧基羰基，羧基等，其表现出强烈的COMT抑制活性。 本发明还提供含有所述化合物的药物组合物及其用途。

公开(公告)号：US20100280083A1

公开(公告)日：2010-11-04

申请号：US12810275

申请日：2008-12-22

申请人： Takehiro Ishikawa ,  Hitoshi Inoue ,  Satoko Kobayashi ,  Masako Yoshida ,  Hiroaki Shiohara ,  Yasunori Ueno ,  Nobuyuki Tanaka

发明人： Takehiro Ishikawa ,  Hitoshi Inoue ,  Satoko Kobayashi ,  Masako Yoshida ,  Hiroaki Shiohara ,  Yasunori Ueno ,  Nobuyuki Tanaka

IPC分类号： A61K31/4245 ,  C07D271/06 ,  C07D413/04 ,  C07D417/10 ,  A61K31/427 ,  A61P25/16

CPC分类号： C07D271/06 ,  C07D413/04 ,  C07D413/10 ,  C07D417/10

摘要： The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is halo-lower alkyl, lower acyl, halo-lower alkylcarbonyl, cycloalkylcarbonyl, optionally substituted arylcarbonyl, lower alkoxycarbonyl or the like; R4 is lower alkyl, halo-lower alkyl, cycloalkyl, lower alkoxy-lower alkyl or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

摘要翻译： 本发明提供由通式（I）表示的化合物或其药学上可接受的盐，其中R 1和R 2各自为氢，低级酰基，低级烷氧基羰基等; 低级酰基，卤代低级烷基羰基，环烷基羰基，任意取代的芳基羰基，低级烷氧基羰基等; R4是表现出强大的COMT抑制活性的低级烷基，卤代低级烷基，环烷基，低级烷氧基 - 低级烷基等。 本发明还提供含有所述化合物的药物组合物及其用途。

公开(公告)号：US08258162B2

公开(公告)日：2012-09-04

申请号：US13002475

申请日：2009-06-26

申请人： Takehiro Ishikawa ,  Satoko Kobayashi ,  Hitoshi Inoue ,  Yasunori Ueno ,  Masako Yoshida ,  Nobuyuki Tanaka

发明人： Takehiro Ishikawa ,  Satoko Kobayashi ,  Hitoshi Inoue ,  Yasunori Ueno ,  Masako Yoshida ,  Nobuyuki Tanaka

IPC分类号： A61K31/04 ,  A61K31/426 ,  A61K31/42 ,  A61K31/381 ,  C07C205/06 ,  C07D277/20 ,  C07D261/06 ,  C07D333/02

CPC分类号： C07C205/61 ,  A61K31/192 ,  A61K31/24 ,  A61K31/277 ,  A61K31/351 ,  A61K31/381 ,  A61K31/40 ,  A61K31/42 ,  A61K31/425 ,  A61K31/4453 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/55 ,  A61K45/06 ,  C07C255/56 ,  C07C255/57 ,  C07C259/10 ,  C07C2601/14 ,  C07C2601/18 ,  C07D261/08 ,  C07D277/24 ,  C07D295/10 ,  C07D309/06 ,  C07D333/22 ,  A61K2300/00

摘要： The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

摘要翻译： 本发明提供由通式（I）表示的化合物或其药学上可接受的盐，其中R 1和R 2各自为氢，低级酰基，低级烷氧基羰基等; R 3是低级烷基，卤素 - 低级烷基，环烷基，杂环烷基，任选取代的芳基，任选取代的杂芳基等; R4是氰基，低级烷氧基羰基，羧基等，其表现出强烈的COMT抑制活性。 本发明还提供含有所述化合物的药物组合物及其用途。

公开(公告)号：US07402692B2

公开(公告)日：2008-07-22

申请号：US11923067

申请日：2007-10-24

申请人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

发明人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

IPC分类号： C07C229/00 ,  C07C69/76

CPC分类号： C07C217/60 ,  C07C43/315 ,  C07C69/712 ,  C07C213/02

摘要： The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has β3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates

摘要翻译： 本发明提供由通式（I）等表示的新型中间体，其用于制备具有β3肾上腺素受体刺激活性并用于治疗或预防肥胖的通式（X）表示的苯氧基乙酸衍生物或其药学上可接受的盐 ，高血糖症，由肠蠕动过多引起的疾病，尿尿症，尿失禁，抑郁症或胆道结石。 本发明还提供了制备所述中间体的方法和使用所述中间体的方法

公开(公告)号：US20060135605A1

公开(公告)日：2006-06-22

申请号：US10526660

申请日：2002-09-05

申请人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

发明人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

IPC分类号： A61K31/235 ,  C07C69/76

CPC分类号： C07C217/60 ,  C07C43/315 ,  C07C69/712 ,  C07C213/02

摘要： The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has β3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates.

摘要翻译： 本发明提供由通式（I）等表示的新型中间体，其用于制备具有β3肾上腺素受体刺激活性并用于治疗或预防肥胖的通式（X）表示的苯氧基乙酸衍生物或其药学上可接受的盐 ，高血糖症，由肠蠕动过多引起的疾病，尿尿症，尿失禁，抑郁症或胆道结石。 本发明还提供了制备所述中间体的方法和使用所述中间体的方法。

公开(公告)号：US20080045739A1

公开(公告)日：2008-02-21

申请号：US11923067

申请日：2007-10-24

申请人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

发明人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

IPC分类号： C07C229/02

CPC分类号： C07C217/60 ,  C07C43/315 ,  C07C69/712 ,  C07C213/02

摘要： The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has β3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates.

摘要翻译： 本发明提供由通式（I）等表示的新型中间体，其用于制备具有β3肾上腺素受体刺激活性并用于治疗或预防肥胖的通式（X）表示的苯氧基乙酸衍生物或其药学上可接受的盐 ，高血糖症，由肠蠕动过多引起的疾病，尿尿症，尿失禁，抑郁症或胆道结石。 本发明还提供了制备所述中间体的方法和使用所述中间体的方法。

公开(公告)号：US20080045741A1

公开(公告)日：2008-02-21

申请号：US11923149

申请日：2007-10-24

申请人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

发明人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

IPC分类号： C07C69/708

CPC分类号： C07C217/60 ,  C07C43/315 ,  C07C69/712 ,  C07C213/02

摘要： The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has β3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates.

公开(公告)号：US07329771B2

公开(公告)日：2008-02-12

申请号：US10526660

申请日：2002-09-05

申请人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

发明人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

IPC分类号： C07C69/76 ,  A01N37/10 ,  A61K31/235

CPC分类号： C07C217/60 ,  C07C43/315 ,  C07C69/712 ,  C07C213/02

摘要： The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has β3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates.

摘要翻译： 本发明提供由通式（I）等表示的新型中间体，其用于制备具有β3肾上腺素受体刺激活性并用于治疗或预防肥胖的通式（X）表示的苯氧基乙酸衍生物或其药学上可接受的盐 ，高血糖症，由肠蠕动过多引起的疾病，尿尿症，尿失禁，抑郁症或胆道结石。 本发明还提供了制备所述中间体的方法和使用所述中间体的方法。

公开(公告)号：US07396954B2

公开(公告)日：2008-07-08

申请号：US11923093

申请日：2007-10-24

申请人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

发明人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

IPC分类号： C07C69/76 ,  A01N37/10 ,  A61K31/235

CPC分类号： C07C217/60 ,  C07C43/315 ,  C07C69/712 ,  C07C213/02

摘要： The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has β3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates

摘要翻译： 本发明提供由通式（I）等表示的新型中间体，其用于制备具有β3肾上腺素受体刺激活性并用于治疗或预防肥胖的通式（X）表示的苯氧基乙酸衍生物或其药学上可接受的盐 ，高血糖症，由肠蠕动过多引起的疾病，尿尿症，尿失禁，抑郁症或胆道结石。 本发明还提供了制备所述中间体的方法和使用所述中间体的方法